Neratinib derivative 7A induces apoptosis in colon cancer cells via the p53 pathway.

Bioorg Med Chem Lett

College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China; College of Pharmacy and Chemistry and Chemical Engineering, Taizhou University, Taizhou, 225 300, China. Electronic address:

Published: December 2024

AI Article Synopsis

  • Colorectal cancer is increasingly becoming a major health concern, prompting the need for new treatments.
  • Recent studies identified a compound called 7A, derived from Neratinib, which shows strong anti-cancer properties but needs further investigation in this specific type of cancer.
  • This research demonstrates that 7A causes DNA damage, triggers the P53 pathway to induce cell death, and reduces both tumor growth and blood vessel formation, suggesting its potential as a new treatment option for colorectal cancer.

Article Abstract

Colorectal cancer remains a significant health threat, with its incidence continuously rising, underscoring the urgent need for the development of new therapeutic agents. In our previous research, we identified 7A, a derivative of Neratinib, as having pronounced antitumor activity. However, its specific effects and mechanisms in colorectal cancer have not been thoroughly investigated. Therefore, this study employed in vivo and in vitro experiments, utilizing techniques such as RNA sequencing, Western blotting, and PCR, to provide a comprehensive analysis of 7A's mechanism of action in colorectal cancer. The results indicate that 7A induces DNA damage and activates the P53 pathway, thereby promoting apoptosis in colorectal cancer cells. Additionally, 7A treatment significantly reduced angiogenesis and tumor weight. Our findings suggest that 7A, a Neratinib derivative, holds promise as a novel candidate for colorectal cancer therapy.

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http://dx.doi.org/10.1016/j.bmcl.2024.130069DOI Listing

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